Tuesday, April 30, 2019

Gleevac Essay Example | Topics and Well Written Essays - 3000 words

Gleevac - Essay ExampleIt has four pKa values 1.52, 2.56, 3.73, 8.07, very fat-soluble in buffers of PH 5.5 and slightly soluble in neutral/alkaline aqueous buffers. Gleevec recognizes the auto repressing conformation of the activation loop of the protein that regulates the kinase activity. The structure of inactive state is distinct between different kinases. It has a half-life of 15 hours and allows daily administration.Gleevec is used to treat the continuing phase of CML though applications have been launch in Advanced and blast crisis phases. Its efficacy has been found to reduce with phase progression.Most patients that dont act to gleevec are in advanced stages of CML at the initiation of treatment. Failure rate of imatinib in patient with chronic phase CML remains low(at less than 15%at 18 months) in patients who did not respond to interferon.In the 1980s and 90s much skepticism prevailed first on the development of compounds with specificity among protein kinases. Second ly, the targeting of singular molecular(a) defects seemed insufficient in the treatment of highly heterogeneous cancer 11. Gazit in 1989 account low molecular weight tyrosine kinase inhibitors with selective activity towards EGFR. These inhibitors were called tyrophostins. Tyrophostins were useful in selective antiproliferation agents for proliferative diseases caused by hyperactivity of protein tyrosine kinases. Though tyrophostins were not clinically developed, they provided the proof of the principle of selective inhibition of tyrosine kinases by using small molecules 16. Subsequently 2 phenylaminopyrimidines were reported as selective inhibitors for protein kinases C (PKC), Abelson (ABL) and platelet derived growth factor receptor (PDGFR) kinases 3. Tyrosine kinases mediate many of the foretoken pathways by which cancer cells promote their proliferation and survival. They control cellular function and are thought to be also similar to be inhibited in-vivo 15. Overall imatini b shows

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